| Literature DB >> 24900562 |
Dean G Brown1, Peter R Bernstein1, Ye Wu1, Rebecca A Urbanek1, Christopher W Becker1, Scott R Throner1, Bruce T Dembofsky1, Gary B Steelman1, Lois A Lazor1, Clay W Scott1, Michael W Wood1, Steven S Wesolowski1, David A Nugiel1, Stephanie Koch1, Jian Yu1, Donald E Pivonka1, Shuang Li1, Carol Thompson1, Anna Zacco1, Charles S Elmore1, Patricia Schroeder1, JianWei Liu1, Christopher A Hurley2, Stuart Ward2, Hazel J Hunt2, Karen Williams2, Joseph McLaughlin1, Valerie Hoesch1, Simon Sydserff1, Donna Maier1, David Aharony1.
Abstract
Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin transporters (SERT). Two compounds, 8b and 21a, along with nomifensine were tested in a rodent receptor occupancy study and demonstrated dose-dependent displacement of radiolabeled NET and DAT ligands. These compounds were efficacious in a rat forced swim assay (model of depression) and also had activity in rat spontaneous locomotion assay.Entities:
Keywords: antidepressant; dopamine; norepinephrine; uptake inhibitors
Year: 2012 PMID： 24900562 PMCID： PMC4027539 DOI： 10.1021/ml300262e
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345